An efficient method for acylation of isoquinolines has been developed using alpha-ketoacids under metal-and additive-free conditions in water. The protocol involves C(sp(2))-H functionalization of isoquinolines providing an easy access to C1-benzoylated isoquinolines, which constitute the core structure of a number of biological active compounds and serve as key intermediate in the synthesis of many alkaloids. (C) 2017 Elsevier Ltd. All rights reserved.
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Univ Tehran, Coll Sci, Sch Chem, Tehran 1417614411, IranUniv Tehran, Coll Sci, Sch Chem, Tehran 1417614411, Iran
Kianmehr, Ebrahim
Pakbaznia, Azin
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Univ Tehran, Coll Sci, Sch Chem, Tehran 1417614411, IranUniv Tehran, Coll Sci, Sch Chem, Tehran 1417614411, Iran
Pakbaznia, Azin
Faghih, Nasser
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Univ Tehran, Coll Sci, Sch Chem, Tehran 1417614411, IranUniv Tehran, Coll Sci, Sch Chem, Tehran 1417614411, Iran
Faghih, Nasser
Forournadi, Alireza
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Univ Tehran Med Sci, Fac Pharm, Tehran, Iran
Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran, IranUniv Tehran, Coll Sci, Sch Chem, Tehran 1417614411, Iran